EFFICIENT PEPTIDE COUPLINGS AND THEIR USE IN THE SYNTHESIS AND ISOLATION OF A CYCLOPENTA (G) QUINAZOLINE TRISODIUM SALT

A new method for the synthesis of L-Glutamyl-?-D-Glutamic acid and its use in the synthesis of (2R)-((4S)-carboxy-4-(4,N-(((6S)-2-(hydroxymethyl)-4-oxo-3,4,7,8- tetrahydro-3H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino)benzamido) butanamido)pentanedioic acid, 1 are provided. Also provided is...

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Hauptverfasser: DALZIEL, SEAN, MARK, JACKS, THOMAS, ELLIOTT, THOMPSON, ANDREW, S, ZELLER, JAMES, ROBERT, CHOUBAL, MILIND, D, KERSCHEN, JAMES, ALAN, BRIDGES, ALEXANDER, JAMES
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creator DALZIEL, SEAN, MARK
JACKS, THOMAS, ELLIOTT
THOMPSON, ANDREW, S
ZELLER, JAMES, ROBERT
CHOUBAL, MILIND, D
KERSCHEN, JAMES, ALAN
BRIDGES, ALEXANDER, JAMES
description A new method for the synthesis of L-Glutamyl-?-D-Glutamic acid and its use in the synthesis of (2R)-((4S)-carboxy-4-(4,N-(((6S)-2-(hydroxymethyl)-4-oxo-3,4,7,8- tetrahydro-3H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino)benzamido) butanamido)pentanedioic acid, 1 are provided. Also provided is an efficient method for the isolation and purification of the trisodium salt of the abovementioned acid, 2, in a form suitable for long term storage and use in a parenteral dosing form. L'invention concerne un nouveau procédé pour la synthèse d'acide L-glutamyl-?-D-glutamique et son utilisation dans la synthèse d'acide (2R)-((4S)-carboxy-4-(4,N-(((6S)-2-(hydroxyméthyl)-4-oxo-3,4,7,8-tétrahydro-3H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino)benzamido)butanamido)pentanedioïque, 1. L'invention concerne également un procédé efficace pour l'isolement et la purification du sel trisodique de l'acide mentionné ci-dessus, 2, dans une forme adaptée pour un stockage à long terme et une utilisation dans une forme posologique parentérale.
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Also provided is an efficient method for the isolation and purification of the trisodium salt of the abovementioned acid, 2, in a form suitable for long term storage and use in a parenteral dosing form. L'invention concerne un nouveau procédé pour la synthèse d'acide L-glutamyl-?-D-glutamique et son utilisation dans la synthèse d'acide (2R)-((4S)-carboxy-4-(4,N-(((6S)-2-(hydroxyméthyl)-4-oxo-3,4,7,8-tétrahydro-3H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino)benzamido)butanamido)pentanedioïque, 1. 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Also provided is an efficient method for the isolation and purification of the trisodium salt of the abovementioned acid, 2, in a form suitable for long term storage and use in a parenteral dosing form. L'invention concerne un nouveau procédé pour la synthèse d'acide L-glutamyl-?-D-glutamique et son utilisation dans la synthèse d'acide (2R)-((4S)-carboxy-4-(4,N-(((6S)-2-(hydroxyméthyl)-4-oxo-3,4,7,8-tétrahydro-3H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino)benzamido)butanamido)pentanedioïque, 1. L'invention concerne également un procédé efficace pour l'isolement et la purification du sel trisodique de l'acide mentionné ci-dessus, 2, dans une forme adaptée pour un stockage à long terme et une utilisation dans une forme posologique parentérale.</abstract><oa>free_for_read</oa></addata></record>
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
title EFFICIENT PEPTIDE COUPLINGS AND THEIR USE IN THE SYNTHESIS AND ISOLATION OF A CYCLOPENTA (G) QUINAZOLINE TRISODIUM SALT
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